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Kinetic parameters for substrate hydrolysis and inhibition of darunavir and saquinavir.
| Mutant | Km (μM) | kcat (/min) | kcat /Km (/min.μM) | Relative kcat/ Km | Ki (nM) | Relative Ki | Ki (nM) | Relative Ki |
|---|---|---|---|---|---|---|---|---|
| DRV | SQV | |||||||
| PR | 30±5 | 194±23 | 7.4±1.2 | 1.0 | 0.58±0.10 | 1 | 0.42±0.07 | 1 |
| PRG48V | 91±8 | 220±9 | 2.4±0.2 | 0.3 | 17±2 | 29 | 36±3 | 86 |
| PRI50V | 109±4 | 68±2 | 0.62±0.02 | 0.1 | 18±1 | 31 | 10±1 | 24 |
| PRI54V | 43±9 | 134±28 | 3.1±0.7 | 0.4 | 5±1 | 8 | 6±1 | 15 |
| PRI54M | 41±3 | 301±22 | 7.3±0.5 | 1.0 | 1.6±0.1 | 3 | 2.2±0.3 | 5 |
